ChemMedChem,
Journal Year:
2024,
Volume and Issue:
19(22)
Published: Sept. 20, 2024
Mycobacteria
are
opportunistic
intracellular
pathogens
that
have
plagued
humans
and
other
animals
throughout
history
still
today.
They
manipulate
hijack
phagocytic
cells
of
immune
systems,
enabling
them
to
occupy
this
peculiar
infection
niche.
exploit
a
plethora
mechanisms
resist
antimicrobials
(e.
g.,
waxy
cell
walls,
efflux
pumps,
target
modification,
biofilms,
etc.)
thereby
evolving
into
superbugs,
such
as
extensively
drug-resistant
tuberculosis
(XDR
TB)
bacilli
the
emerging
pathogenic
Mycobacterium
abscessus
complex.
This
review
summarizes
action
some
surging
antimycobacterial
strategies.
Exploiting
fact
mycobacteria
obligate
aerobes
differences
between
their
oxidative
phosphorylation
pathways
versus
human
counterpart
opens
promising
avenue
for
drug
discovery.
The
polymorphism
respiratory
complexes
across
mycobacterial
imposes
challenges
on
repositioning
agents
battle
rise
in
nontuberculous
infections.
In
silico
strategies
exploiting
machinery
data
design
novel
therapeutic
touched
upon.
potential
druggability
elements
is
reviewed.
Future
research
addressing
health
associated
with
discussed.
Angewandte Chemie,
Journal Year:
2025,
Volume and Issue:
unknown
Published: March 6, 2025
Abstract
Z‐DNA
binding
protein
1
(ZBP1)
has
emerged
as
a
critical
pathogen‐sensing
that
upon
activation,
triggers
necroptotic
signaling
cascades,
leading
to
potent
inflammatory
response
and
potentially
causing
significant
tissue
damage.
However,
available
drugs
specifically
developed
for
the
effective
inhibition
or
degradation
of
ZBP1
is
still
lacking
so
far.
In
this
study,
we
covalent
recognition‐based
PROTAC
(C‐PROTAC)
molecule
ZBP1.
It
consists
DNA
aptamer
recognition
moiety
an
E3
enzyme‐recruiting
unit,
connected
by
linker
containing
N
‐acyl‐
‐alkyl
sulfonamides
(NASA)
groups.
The
binds
ZBP1,
while
NASA‐containing
facilitates
formation
bond
between
target
protein.
ligase‐recruiting
unit
then
directs
ubiquitin‐proteasome
system
degrade
ZBP1‐PROTAC
complex.
This
approach
combines
high
specificity
aptamers
with
efficiency
degradation‐inducing
capabilities
PROTACs,
providing
powerful
tool
targeted
degradation.
successful
application
technology
highlights
its
potential
selective
elimination
disease‐associated
proteins
development
novel
therapeutic
strategies.
Biomaterials Science,
Journal Year:
2024,
Volume and Issue:
12(14), P. 3686 - 3699
Published: Jan. 1, 2024
A
near-infrared
light-controlled
PROTAC
delivery
nanodevice
achieves
enhanced
protein
degradation
efficiency
and
synergistic
therapeutic
efficacy
in
combination
with
NIR
light-triggered
photodynamic
therapy.
Pharmaceuticals,
Journal Year:
2025,
Volume and Issue:
18(3), P. 297 - 297
Published: Feb. 21, 2025
Absorption
and
permeability
are
critical
physicochemical
parameters
that
must
be
balanced
to
achieve
optimal
drug
uptake.
These
key
factors
closely
linked
the
maximum
absorbable
dose
required
provide
appropriate
plasma
levels
of
drugs.
Among
various
strategies
employed
enhance
solubility
permeability,
prodrug
design
stands
out
as
a
highly
effective
versatile
approach
for
improving
properties
enabling
optimization
biopharmaceutical
pharmacokinetic
while
mitigating
adverse
effects.
Prodrugs
compounds
with
reduced
or
no
activity
that,
through
bio-reversible
chemical
enzymatic
processes,
release
an
active
parental
drug.
The
application
this
technology
has
led
significant
advancements
in
during
phase,
it
offers
broad
potential
further
development.
Notably,
approximately
13%
drugs
approved
by
U.S.
Food
Drug
Administration
(FDA)
between
2012
2022
were
prodrugs.
In
review
article,
we
will
explore
describing
examples
market
We
also
describe
use
optimize
PROteolysis
TArgeting
Chimeras
(PROTACs)
using
conjugation
technologies.
highlight
some
new
technologies
prodrugs
enrich
properties,
contributing
developing
safe
Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Sept. 13, 2024
Emerging
drug
candidates
more
often
fall
in
the
beyond-rule-of-five
chemical
space.
Among
them,
proteolysis
targeting
chimeras
(PROTACs)
have
gained
great
attention
past
decade.
Although
physicochemical
properties
of
small
molecules
accomplishing
Lipinski's
rule-of-five
can
now
be
easily
predicted
through
models
generated
by
large
data
collections,
for
PROTACs
knowledge
is
still
limited
and
heterogeneous,
hampering
their
prediction.
Here,
kinetic
solubility
coefficient
distribution
at
pH
7.4
(LogD
